Anti-obesity and anti-diabetic effects of CL316,243, a highly specific beta 3-adrenoceptor agonist, in Otsuka Long-Evans Tokushima Fatty rats: induction of uncoupling protein and activation of glucose transporter 4 in white fat.
Anti-obesity and anti-diabetic effects of CL316,243, a highly specific beta 3-adrenoceptor agonist, in Otsuka Long-Evans Tokushima Fatty rats: induction of uncoupling protein and activation of glucose transporter 4 in white fat.
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CL316,243（一种高度特异性 β3-肾上腺素受体激动剂）对大冢 Long-Evans 德岛脂肪大鼠的抗肥胖和抗糖尿病作用：诱导白色脂肪中的解偶联蛋白和激活葡萄糖转运蛋白 4。
DOI：
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发表时间：
1997
影响因子：
5.8
通讯作者：
Motoharu Kondo
中科院分区：
文献类型：
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作者：
T. Umekawa;Toshihide Yoshida;Naoki Sakane;Masayuki Saito;Kenzo Kumamoto;Motoharu Kondo
在大冢Long-Evans德岛肥胖大鼠（肥胖）和Long-Evans德岛大冢大鼠（对照）中研究了高度特异性β 3肾上腺素受体激动剂CL 316，243（CL; β 1：β 2：β 3 = 0：1：100，000）的抗肥胖和抗糖尿病作用。每日注射CL（0.1 mg/kg，s.c.）对这些大鼠（10周龄）进行14周的处理导致体重显著降低（脂肪，27%;对照，15%），与脂肪垫重量显著降低（腹股沟：脂肪，60%;对照，36%;腹膜后：脂肪，75%;对照，77%）相关，而不影响食物摄取。解偶联蛋白的mRNA水平和解偶联蛋白（UCP）的蛋白水平，以及棕色脂肪组织中的鸟苷5 '-二磷酸结合（产热的可靠指标），在脂肪大鼠中低于对照组。然而，CL治疗后，两组棕色脂肪组织中的这些参数均显著增加2至3倍。此外，解偶联蛋白在白色脂肪组织以及棕色脂肪组织中被诱导。肥胖大鼠在糖耐量试验中出现高血糖和高胰岛素血症，但CL可改善这些参数。这些结果表明，棕色脂肪组织产热减少可能是肥胖大鼠肥胖的原因之一，CL给药通过减少白色脂肪量、激活棕色脂肪组织产热和诱导白色脂肪组织解偶联蛋白来预防肥胖。此外，CL治疗可通过改善肥胖和激活白色脂肪组织和棕色脂肪组织中的葡萄糖转运蛋白4来抑制糖尿病。
The anti-obesity and anti-diabetic effects of a highly specific beta 3-adrenoceptor agonist, CL316,243 (CL; beta 1: beta 2: beta 3 = 0:1:100,000), were investigated in Otsuka Long-Evans Tokushima Fatty (fatty) and Long-Evans Tokushima Otsuka (control) rats. Daily injection of CL (0.1 mg/kg, s.c.) to these rats (10 weeks old) for 14 weeks caused a significant reduction in body weight (fatty, 27%; control, 15%), associated with a marked decrease in fat pad weight (inguinal: fatty, 60%; control, 36%; retroperitoneal: fatty, 75%; control, 77%) without affecting food intake. The levels of uncoupling protein mRNA and protein levels of uncoupling protein (UCP), as well as guanosine 5'-diphosphate-binding (a reliable index of thermogenesis) in brown adipose tissue, were lower in the fatty than in the control rats. However, after CL treatment, these parameters in brown adipose tissue increased significantly 2- to 3-fold in both groups. Furthermore, uncoupling protein was induced in white adipose tissue as well as in brown adipose tissue. The fatty rats showed hyperglycemia and hyperinsulinemia during the glucose tolerance test, but CL ameliorated these parameters. These findings suggest that decreased thermogenesis in brown adipose tissue may be one of the causes of obesity in the fatty rats and that administration of CL prevents obesity by decreasing white fat mass, by activating brown adipose tissue thermogenesis, and by inducing uncoupling protein in white adipose tissue. Furthermore, CL treatment may inhibit diabetes mellitus by ameliorating obesity and by activating glucose transporter 4 in white adipose tissue and brown adipose tissue.
影响因子：
158.5
作者：
WALSTON, J;SILVER, K;SHULDINER, AR
通讯作者：
SHULDINER, AR
影响因子：
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作者：
HIMMSHAGEN, J;CUI, JY;CLAUS, TH
通讯作者：
CLAUS, TH